LY-404187 是有效的，选择性和中枢活性的 AMPA 受体的正变构调节剂，作用于 GluR1i，GluR2i，GluR2o，GluR3i 和 GluR4i 的 EC₅₀ 值分别为 5.65、0.15、1.44、1.66 和 0.21 µM。LY-404187 有潜力用于许多精神疾病和神经退行性疾病的研究。

LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC 50 s of 5.65, 0.15, 1.44, 1.66 and 0.21 μM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.

Solid

EC50: 5.65 μM (GluR1i), 0.15 μM (GluR2i), 1.44 μM (GluR2o), 1.66 μM (GluR3i), 0.21 μM (GluR4i)

LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells.
LY-404187 (0.03-10 μM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC50=1.3±0.3 μM) and efficacy (Emax=45.3±8.0-fold increase) .
LY-404187 does not affect the magnitude or time course of wholecell K or Na currents in pre frontal cortex (PFC) pyramidal neurons at concentrations of 10 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice.
LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies.
LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats.
LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death.
LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Quirk JC, et, al. LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. Fall 2002; 8(3): 255-82.
[2]. Miu P, et, al. Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology. 2001 Jun; 40(8): 976-83.

In Vitro: DMSO : 100 mg/mL (292.00 mM; Need ultrasonic)配制储备液